Tetrasubstituted 2-acetylthiophene derivative 5 was synthesized and then condensed with various nitrogen nucleophiles such as 5-amino-1,2,4-triazole, 2-aminobenzimidazole, aniline or p-chloroaniline to afford the corresponding iminothiophene derivatives 6-8a,b. Condensation of thiophene 5 with malononitrile as carbon nucleophile afforded compound 9, which underwent nucleophilic addition with DMF-DMA to afford compound 10. The newly synthesized products were characterized by elemental analysis, IR, MS, 1 H-13 C-NMR and CHN analysis and then evaluated for their antimicrobial activity. Results of the in vitro antibacterial activity showed that thiophene derivative 7 was found to be more potent than the standard drug gentamicin against Pseudomonas aeruginosa. Some of these compounds showed potential antimicrobial activities. Molecular docking and Osiris/Molinspiration analyses show the crucial role and impact of substituents on bioactivity and indicate the unfavorable structural parameters in actual drug design: more substitution with electronic donor group doesn't guarantee more effective bioactivity. This study should greatly help in an intelligent and a controlled pharmacomodulation of antibiotics.
Medicinal and food plants as well as their bioactive fractions have been used by diverse human cultures since ancient times. These plants provide multiple health benefits because of the presence of a plethora of phytochemicals including phenylpropanoids, isoprenoids, alkaloids, sulphated compounds, peptides and polysaccharides that are responsible for various biological activities such as anticancer, antioxidant, antifungal, antibacterial, anti-dysenteric, anti-inflammatory, antiulcer, anti-hypertensive and anticoagulant properties. The genus Rumex includes edible and medicinal herbs belonging to buckwheat (Polygonaceae) family, consisting of about 200 species rich in phenylpropanoids and anthraquinones. Some Rumex species have exhibited health-promoting effects and have been used as traditional foods and herbal remedies, though a limited information has been documented on their specific biological properties. Therefore, this survey aimed at reviewing the Rumex species with documented biological activity, focusing on preclinical evidences on their efficacy and safety.
Exposure of heavy metals to human beings has risen dramatically in the last 50 years. In today's urban and industrial society, there is no escaping from exposure to toxic chemicals and heavy metals. Humans are more likely to be exposed to heavy metal contamination from the dust that adheres to edible plants than from bioaccumulation. This is because it is very difficult to wash off all the dust particles from the plant material before ingesting them. The objectives of this experiment were to determine the concentrations of lead (Pb) and cadmium (Cd) in washing residues and in the tissues of fruits of date palm growing in 14 sites of Riyadh and also to assess whether the fruits were safe for human consumption. The washing residues and tissue of date palm fruits collected from different sites showed the presence of significant amounts of the Pb and Cd. The concentration of Pb in the dust and fruit tissue increased with increasing anthropogenic sources. Therefore, fruits of date palm might be used as a pollution indicator; it might be recommend that fruits of date palm could be safe for human consumption after washing. The mean concentration of Pb and Cd in all the samples collected from different sites is within the safe limits recommended by FAO/WHO.
Ethyl 5-acetyl-4-methyl-2-(phenylamino)thiophene-3-carboxylate (2) and there derivatives 3a-c, 4, 6a-c and 9a-f were synthesized. The structure of compound 2 was deduced by
8713Compound 3c was also more potent (MIC 24.8 ± 0.64) than the standard drug amphotericin B (MIC 19.7 ± 0.2) against Syncephalastrum racemosum. Compounds 4 and 9f also showed promising anti-microbial activity. Molecular modeling was performed for the most active compounds.
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